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82

B.E. McCarey

Table 3.3  The peak fluorescein values as measure with the fluorophotometer following­ topical application of fluorescein to the treated eye

 

Cornea

 

Retina

 

 

 

 

 

 

 

 

Treatment

Contralateral

Treatment

Contralateral

 

(ng/mL)

(ng/mL)

(ng/mL)

(ng/mL)

Autofluorescence

  14

11.1

6.0

4.8

Post-75 min

335

11.5

5.2

4.9

Post-255 min

191.9

15.5

8.2

4.0

topical applications of fluorescein. The experiment supports the difficulty of delivering­ fluorescein to the posterior segment of the eye with topical corneal applications.

References

Adler CA, Maurice DM, Paterson ME (1971) The effect of viscosity of the vehicle on the penetration of fluorescein into the human eye. Exp Eye Res 11:34–42

Araie M (1986) Carboxyfluorescein. A dye for evaluating the corneal endothelial barrier function in vivo. Exp Eye Res 42:141–150

Araie M, Maurice D (1987) The rate of diffusion of fluorophores through the corneal epithelium and stroma. Exp Eye Res 44:73–87

Berkowitz RA, Klyce SD, Salisbury JD, Kaufman HE (1981) Fluorophotometric determination of the corneal epithelial barrier after penetrating keratoplasty. Am J Ophthalmol 92:332–335

Boets EP, van Best JA, Boot JP, Oosterhuis JA (1988) Corneal epithelial permeability and daily contact lens wear as determined by fluorophotometry. Curr Eye Res 7:511–514

Bron AJ (1985) Prospects for the dry eye. Trans Am Ophthalmol Soc 104:801–811

Burstein NL (1980) Preservative cytotoxic threshold for benzalkonium chloride and chlorhexidine in cat and rabbit corneas. Invest Ophthalmol Vis Sci 19:308–813

Burstein NL (1984) Preservative alteration of corneal permeability in humans and rabbits. Invest Ophthalmol Vis Sci 25:1453–1457

Burstein NL, Klyce SD (1977) Electrophysiologic and morphologic effects of ophthalmic preparations on rabbit cornea epithelium. Invest Ophthalmol Vis Sci 16:899–911

Cadwallader DE, Ansel HC (1965) Hemolysis of erythrocytes by antibacterial preservatives. II. Quarternary ammonium salts. J Pharm Sci 54:1010–1012

Champeau EJ, Edelhauser HF (1986) Effects of ophthalmic preservatives on the ocular surface: conjunctiva and corneal uptake and distribution of benzalkonium chloride and chlorhexidine digluconate. In: Holly FJ (ed) The preocular tear film: in health, disease, and contact lens wear. Dry Eye Institute, Lubbock, TX, pp 292–302

Chang SW, Hu FR (1993) Changes in corneal autofluorescence and corneal epithelial barrier function with aging. Cornea 12:493–499

Chang SW, Hsu HC, Hu FR, Chen MS (1995) Corneal autofluorescence and epithelial barrier function in diabetic patients. Ophthalmic Res 27:74–79

Cunha-Vaz J, de Abreu J, Campos A (1975) Early breakdown of the blood-retinal barrier in diabetes. Br J Ophthalmol 59:649–656

de Kruijf EJ, Boot JP, Laterveer L, van Best JA, Ramselaar JA, Oosterhuis JA (1987) A simple method for determination of corneal epithelial permeability in humans. Curr Eye Res 6:1327–1334

Forster S, Mead A, Sears M (1979) An interophthalmic communicating artery as explanation for the consensual irritative response of the rabbit eye. Invest Ophthalmol Vis Sci 18:161–165

3Fluorophotometry for Pharmacokinetic Assessment

83

Gobbels M, Spitznas M (1991) Effects of artificial tears on corneal epithelial permeability in dry eyes. Graefes Arch Clin Exp Ophthalmol 229:345–349

Gobbels M, Spitznas M (1992) Corneal epithelial permeability of dry eyes before and after treatment with artificial tears. Ophthalmology 99:873–878

Gobbels M, Spitznas M, Oldendoerp J (1989) Impairment of corneal epithelial barrier function in diabetics. Graefes Arch Clin Exp Ophthalmol 227:142–144

Gobbles M, Spitznas M (1989) Influence of artificial tears on corneal epithelium in dry eye syndrome. Graefes Arch Clin Exp Ophthalmol 227:139–141

Gray JR, Mosier MA, Ishimoto BM (1985) Optimized protocol for Fluorotron Master. Graefes Arch Clin Exp Ophthalmol 222:225–229

Grimes PA, Stone RA, Laties AM, Li W (1982) Carboxyfluorescein. A probe of the blood ocular barriers with lower membrane permeability than fluorescein. Arch Ophthalmol 100:635–639

Hughes L, Maurice D (1984) A fresh look at iontophoresis. Arch Ophthalmol 102:1825–1829 Jones RF, Maurice DM (1966) New methods of measuring the rate of aqueous flow on man with

fluorescein. Exp Eye Res 5:208–220

Joshi A, Maurice D, Paugh JR (1996) A new method for determining corneal epithelial barrier to fluorescein in humans. Invest Ophthalmol Vis Sci 37:1008–1016

Kanno Y, Loewenstein WR (1964) Intercellular diffusion. Science 143:959–960

Kuppens EVM, Stolwijk TR, de Keizer RJW, van Best JA (1992) Basal tear turnover and topical timolol in glaucoma patients and healthy controls by fluorophotometry. Invest Ophthalmol Vis Sci 33:3442–3448

Kuppens E, Stolwijk T, van Best J, de Keizer R (1994) Topical timolol, corneal epithelial permeability and autofluorescence in glaucoma by fluorophotometry. Graefes Arch Clin Exp Ophthalmol 232:215–220

Lin MC, Graham AD, Fusaro RE, Polse KA (2002) Impact of rigid gas-permeable contact lens extended wear on corneal epithelial barrier function. Invest Ophthalmol Vis Sci 43:1019–1024

Maurice D (1963) A new objective fluorophotometer. Exp Eye Res 2:33–38

McCarey BE, al Reaves T (1995) Noninvasive measurement of corneal epithelial permeability. Curr Eye Res 14:505–510

McCarey BE, Reaves TA (1997) Effect of tear lubricating solutions on in vivo corneal epithelial permeability. Curr Eye Res 16:44–50

McCarey BE, Walter JJ (1998) Ocular fluorophotometry of fluorescein uptake following periorbital injections. Invest Ophthalmol Vis Sci 39:S275

McNamara NA, Fusaro RE, Brand RJ, Polse KA, Srinivas SP (1997) Measurement of corneal epithelial permeability to fluorescein. A repeatability study. Invest Ophthalmol Vis Sci 38:1830–1839

McNamara NA, Polse KA, Bonanno JA (1998) Fluorophotometry in contact lens research: the next step. Optom Vis Sci 75:316–322

Mishima S, Maurice DM (1971) In vivo determination of the endothelial permeability to fluorescein. Acta Soc Ophthalmol 75:236–243

Nelson JD (1995) Simultaneous evaluation of tear turnover and corneal epithelial permeability by fluorophotometry in normal subjects and patients with keratoconjunctivitis sicca (KCS). Trans Am Ophthalmol Soc 93:709–753

Occhipiniti JR, Mosier MA, La Motte J, Monji GT (1988) Fluorophotometric measurement of human tear turnover rate. Curr Eye Res 7:995–1000

OcuMetrics I (1995) FM-2 Fluorotron™ Master, Operators Manual, OcuMetrics, Inc., 2224-C Old Middlefield Way, Mountain View, CA 94043-2421, 650:960–3955

Ota Y, Mishima S, Maurice DM (1974) Endothelial permeability of the living cornea to fluorescein. Invest Ophthalmol Vis Sci 13:945–949

Paugh JR, Joshi A (1992) Novel fluorophotometric methods to evaluate tear flow dynamics in man. Invest Ophthalmol Vis Sci 33:S950

Paugh JR, Saai A, Abhay J (1998) Preservative effect on epithelial barrier function measured with a novel technique. Adv Exp Med Biol 438:731–735

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B.E. McCarey

Pfister RR, Burstein NL (1976) The effects of ophthalmic drugs, vehicles, and preservatives on corneal epithelium: a scanning electron microscope study. Invest Ophthalmol Vis Sci 15:246–259

Ramselaar JA, Boot JP, van Haeringen NJ, van Best JA, Oosterhuis JA (1988) Corneal epithelial permeability after instillation of ophthalmic solutions containing local anesthetics and preservatives. Curr Eye Res 7:947–950

Schalnus R, Ohrloff C (1990) Permeability of the limiting cell layers of the cornea in vivo. Lens Eye Toxic Res 7:371–384

Tognetto D, Cecchini P, Sanguinetti G, Pedio M, Ravalico G (2001) Comparative evaluation of corneal epithelial permeability after the use of diclofenac 0.1% and flurbiprofen 0.03% after phacoemulsification. J Cataract Refract Surg 27:1392–1396

Tsuboti S, Pedersen JE (1987) Acetazolamide effect on the inward permeability of the blood-retina barrier in diabetes. Invest Ophthalmol Vis Sci 28:92–95

van Best J, Tijin A, Tsoi EWSJ, Boets EP, Oosterhuis JA (1985) In vivo assessment of lens transmission for blue-green light by autofluorescence measurement. Ophthalmic Res 17:90–95

van Best JA, Kappelhof JP, Laterveer L, Oosterhuis JA (1987) Blood aqueous barrier permeability verses age by fluorophotometry. Curr Eye Res 6:855–863

van Zutphen H, Demel RA, Norman AW, van Deenen LLM (1971) The action of polyene antibiotics on lipid bilayer membranes in the presence of several cations and anions. Biochim Biophys Acta 241:310–330

Webber W, Jones DP, Wright P (1987) Fluorophotometric measurements of tear turnover rate in normal healthy persons: evidence for a circadian rhythm. Eye 1:615–620

Yokoi K, Yokoi N, Kinoshita S (1998) Impairment of ocular surface epithelium barrier function in patients with atopic dermatitis. Br J Ophthalmol 82:797–800

Zeimer RC, Cunha-Vaz JG, Johnson ME (1982) Studies on the technique of vitreous fluorophotometry. Invest Ophthalmol Vis Sci 22:668–674

Chapter 4

Systemic Route for Retinal Drug Delivery: Role of the Blood-Retinal Barrier

Masanori Tachikawa, Vadivel Ganapathy, and Ken-ichi Hosoya

Abstract  Systemic delivery of therapeutic drugs to the retina is hindered by the presence of the blood-retinal barrier (BRB) which consists of retinal vascular endothelial cells (inner BRB) and retinal pigment epithelial cells (outer BRB). Recent progress in the BRB research has revealed that the BRB expresses a wide variety of transporters essential for the blood-to-retinal influx transport of nutrients and their analogs. At the same time, the BRB also possesses several transporters responsible for the retina-to-blood efflux transport of xenobiotics and drugs, thus being involved in the removal of potentially harmful compounds from the retina. This information can be exploited to our advantage to establish efficient strategies for optimal delivery of clinically relevant therapeutic drugs into the retina.

Abbreviations

 

ABC

ATP-binding cassette

 

AZT

3¢-azido-3¢-deoxythymidine (zidovudine)

 

BAPSG

N-4-benzoylaminophenylsulfonylglycine

 

BCRP

Breast cancer resistance protein

 

BRB

Blood-retinal barrier

 

CRT

Creatine transporter

 

DHA

Dehydroascorbic acid

 

ENT

Equilibrative nucleoside transporter

 

GLUT

Facilitative glucose transporter

 

HDL

High-density lipoprotein

 

 

 

 

K.-i. Hosoya (*)

 

Department of Pharmaceutics, Graduate School of Medicine

 

and Pharmaceutical Sciences, University of Toyama,

 

Toyama 930-0194, Japan

 

e-mail: hosoyak@pha.u-toyama.ac.jp

 

U.B. Kompella and H.F. Edelhauser (eds.), Drug Product Development for the Back of the Eye,

85

AAPS Advances in the Pharmaceutical Sciences Series 2, DOI 10.1007/978-1-4419-9920-7_4,

 

© American Association of Pharmaceutical Scientists, 2011

 

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